GSK-3685032 |
| カタログ番号GC63483 |
GSK-3685032 は、0.036 μM の IC50 を持つ、非時間依存性、非共有結合性、ファーストインクラスの可逆的 DNMT1 選択的阻害剤です。 GSK-3685032 は、DNA メチル化の強力な損失、転写活性化、およびがん細胞増殖阻害を誘導します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2170137-61-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1].
GSK-3685032 (6 days) has cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM[1].GSK-3685032 (0.1-1000 nM, 1-6 days) exhibits growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course[1].GSK3685032 (10-10000 nM, day 4) dose-dependently increases the immune-related gene transcription[1].GSK3685032 (3.2-10,000 nM, 2 days) inhibits DNMT1 protein expression[1].GSK3685032 induces DNA hypomethylation and gene activation[1].
GSK-3685032 (1-45 mg/kg; subcutaneous twice daily for 28 days) inhibits tumor growth in the subcutaneous MV4-11 or SKM-1 xenograft models[1]. Summary of mouse pharmacokinetic parameters for GSK-3685032[1] Dose,Route Cmax(ng/mL) AUC0-8hr(h*ng/mL) DNAUC(h*kg*ng/mL/mg) Clearance(mL/min/kg) Volumedss(L/kg) T1/2(h) 2 mg/kg,IV 5103 2418 1209 13 1.3 1.8 2 mg/kg,SC 252 921 461 NA NA 2.8 2 mg/kg,SC 5473 15400 513 NA NA ND
[1]. Pappalardi MB, et al. Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nat Cancer. 2021;2(10):1002-1017.
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *